489478

LSD1 Inhibitor III, CBB1007

The LSD1 Inhibitor III, CBB1007 controls the biological activity of LSD1. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): LSD1 Inhibitor III, CBB1007, LSD Inhibitor III, BHC110 Inhibitor III, Methyl-3-(4-(4-carbamimidoylbenzoyl)piperazine-1-carbonyl)-5-((4-carbamimidoylpiperazin-1-yl)methyl)benzoate, 3TFA, KDM1 Inhibitor III, Histone Lysine Demethylase Inhibitor V, LSD Inhibitor III, Methyl-3-(4-(4-carbamimidoylbenzoyl)piperazine-1-carbonyl)-5-((4-carbamimidoylpiperazin-1-yl)methyl)benzoate, 3TFA, KDM1 Inhibitor III, Histone Lysine Demethylase Inhibitor V, BHC110 Inhibitor III
• Empirical Formula (Hill Notation): C₂₇H₃₄N₈O₄ · 3C₂HF₃O₂
• CAS Number: 1379573-92-8
• Molecular Weight: 876.68
• MDL number: MFCD25976706
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥99% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: NC(N1CCN(CC2=CC(C(N3CCN(C(C4=CC=C(C(N)=N)C=C4)=O)CC3)=O)=CC(C(OC)=O)=C2)CC1)=N

Description

General description

A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC₅₀ = 5.27 µM for hLSD1) and efficiently blocks LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC₅₀ ≤ 5 µM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC₅₀ ≤ 5 µM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 µM). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC₅₀ >100 µM).

Note: the molecular weight is lot-specific and can be found on the vial label.

A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC₅₀ = 5.27 µM for hLSD1) and efficiently blocks LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC₅₀ ≤ 5 µM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC₅₀ ≤ 5 µM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC₅₀ ≤ 3.74 µM). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC₅₀ >100 µM).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Wang, J., et al. 2011. Cancer Res.71, 7238.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable